MT-SYK-03 is selective orally available inhibitor of cSrc and SYK kinases, inhibits cSrc and SYK with IC50 of 14.2 and 23 nM respectively.
MT-SYK-03 at 500 nM inhibits 34 kinases by more than 50%, 13 kinases by more than 80% and only five kinases by more than 90% in a panel of 341 protein kinases.
MT-SYK-03 effectively suppresses osteoclast-mediated bone resorption and inhibits degradation of aggrecan and type II collagen in chondrocytes.
MT-SYK-03 dose-dependently inhibits anti-IgM induced autophosphorylation of SYK kinase, phosphorylation of downstream B-cell signaling cascade components CD19 and BTK, as well as components of MAP cascade (ERK1/2 and JNK1/2).
MT-SYK-03 inhibits BCR-dependent (but not PMA-dependent) activation of B cells with IC50 of 0.55 uM, inhibits TNF-α release in monocytes with IC50 of 0.48 uM.
MT-SYK-03 shows anti-resorptive effects on cartilage in surgically induced meniscal tear OA in rats.
MT-SYK-03 alleviates inflammation and cartilage damage in murine CIA.